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  • Title: Synthesis of solution-phase phosphoramidite and phosphite ligand libraries and their in situ screening in the rhodium-catalyzed asymmetric addition of arylboronic acids.
    Author: Jagt RB, Toullec PY, Schudde EP, de Vries JG, Feringa BL, Minnaard AJ.
    Journal: J Comb Chem; 2007; 9(3):407-14. PubMed ID: 17430002.
    Abstract:
    Herein, we report the automated parallel synthesis of solution-phase libraries of phosphoramidite ligands for the development of enantioselective catalysts. The ligand libraries are screened in situ in the asymmetric rhodium-catalyzed addition of arylboronic acids to aldehydes and imines. It is shown that the described methodology results in the straightforward discovery of leads for highly efficient enantioselective catalysts.
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